发明申请
- 专利标题: Novel process for preparing 3-fluoroquinolines
- 专利标题(中): 制备3-氟喹啉的新方法
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申请号: US10985533申请日: 2004-11-10
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公开(公告)号: US20050182259A1公开(公告)日: 2005-08-18
- 发明人: Youssef El-Ahmad , Jean-Pierre Leconte , Joel Malpart , Serge Mignani , Stephane Mutti , Michel Tabart
- 申请人: Youssef El-Ahmad , Jean-Pierre Leconte , Joel Malpart , Serge Mignani , Stephane Mutti , Michel Tabart
- 申请人地址: US Antony
- 专利权人: Aventis Pharma S.A.
- 当前专利权人: Aventis Pharma S.A.
- 当前专利权人地址: US Antony
- 优先权: FR0313384 20031117
- 主分类号: C07D215/18
- IPC分类号: C07D215/18 ; C07D215/38 ; C07D215/12
摘要:
The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
公开/授权文献
- US07396934B2 Process for preparing 3-fluoroquinolines 公开/授权日:2008-07-08